3. Introduction
Dosage form (Medicines) API + Excipients
The means (or the form) by which drug molecules are delivered to sites of
action within the body.
Drug (Active pharmaceutical ingredients )
Chemical compound intended for used in diagnosis, treatment prevention,
of disease.
OR
The Active Pharmaceutical Ingredient (API) is the part of any drug that
produces its effects.
Excipients
• do not increase or affect the therapeutic action of the active ingredient,.
• Inactive ingredients may also be referred to as inert ingredients or
excipients, and generally have no pharmacological effect.
• Examples of inactive ingredients include binding materials, dyes,
preservatives, and flavoring agents,sweetening agents,coloring agents etc.
4. Direct clinical use of the active drug substances is rare: Why??
API handling and Accurate dosing can be difficult or
impossible (e.g., potent drugs: low mg and µg doses).
API administration can be impractical/unfeasible because of
size, shape, smell/odour, taste and low activity.
Some API are chemically unstable in light, moisture, O2
API can be degraded at the site of administration (e.g., low pH
in stomach).
API may cause local irritations or injury when they are present
at high concentrations at the site of administration.
Administration of active substance would mean to have no
chance for modification (improvement) of its PK profile.
5. The need for dosage forms:
Accurate dose.
Protection e.g. coated tablets, sealed ampules.
Protection from gastric juice.
Masking taste and odour.
Placement of drugs within body tissues.
Sustained release medication.
Controlled release medication.
Optimal drug action.
Insertion of drugs into body cavities (rectal, vaginal)
Use of desired vehicle for insoluble drugs.
7. Solid dosage forms
• Solid dosage forms are available mostly in unit
dosage forms.
• Some solids are packed and supplied in bulk.
• The bulk forms meant for internal use are supplied
either as granules or fine powder.
• The bulk powder meant for external use are dusting
powder, insufflations, snuffs and tooth powders.
9. Tablets
They are unit solid dosage form consisting of active
ingredients and suitable pharmaceutical excipients.
they may very in size, shape, hardness, thickness, weight,
disintegration,dissolution characterisitics and in other aspect.
10. Capsules
Capsule are solid unit dosage
forms in which one or more
medicaments enclosed within a
shell.
Types –
Hard gelatin capsule
(powder,granules,bead,tablet)
Soft gelatin capsule
(liquids or semisolids)
11. Pills
These are small, rounded solid dosage forms containing
medicaments intended for oral use.
The medicaments are mixed with excipients to forms a firms
plastic mass.
The mass is rolled to uniform pill pipe, which cut into numbers
of uniform pills. The pills are spherical in shape & produced
by rolling them under wooden pill rounder.
12. Lozenge
It is a solid preparation consisting of
sugar and gum & are intended to
dissolve or disintegrate slowly in the
mouth.
It is used to medicate the mouth and
throat for the slow administration of
indigestion or cough remedies.
13. Pastilles
They are solid medicated
preparations designed to
dissolve slowly in the mouth.
They are softer than lozenges
and their bases are either
glycerol and gelatin, or acacia
and sugar.
14. Powder
Powders are solid dosage form of medicaments which are
meant for internal or external use.
They are available in amorphous and crystalline forms.
TYPES OF POWDERS
1. Bulk Powders for internal use e.g. fine powders or granules
2. Bulk Powders for external use e.g. snuff, dusting powders, tooth powder
3. Simple and compound powder for internal use.
4.Powders in the form of compressed tablets and tablet triturates.
5.Powders enclosed in cachets and capsules
15. Dusting powders
These are meant for external application to the skin and are
generally in a very fine state of subdivision to avoid local
irritation.
These are mainly used for their antiseptic, astringent,
absorbent, antiperspirant and antipruritic action.
16. Insufflations
These are medicated dusting powders
meant for introduction into body cavities
(nose, throat, ear, vagina etc) with the
help of an apparatus known as a
insufflator.
It sprays the powders (in a state of fine
particles) on site of application.
17. Snuffs
These are finely divided solid
dosage forms of medicaments
which are inhaled into nostrils.
They are mainly used for their
antiseptic, bronchodilator and
decongestion action.
18. Liquid dosage form
It may be defined as “A solution is a liquid-preparation that contains one or
more soluble chemical substances dissolved in a specified solvent”
Liquid dosage forms are intended for External, Internal or parenteral use.
They mainly classified into two category namely as –
I) Internal Liquid Preparations.
A) Monophasic liquid preparations
B) Biphasic liquid preparations
II) External Liquid Preparations
A) Applied on the skin
B) Instilled into body cavities
C) Used in mouth
19. Advantage
Immediately available for absorption.
Administration convenient, particularly for infants, psychotic
patients.
Easy to color, flavor & sweeten.
Liquids are easier to swallow than solids and are therefore
particularly acceptable for pediatric patient.
A solution is an homogeneous system and therefore the drug
will be uniformly distributed throughout the preparation.
Some drugs like aspirin, KCl can irritate gastric mucosa if
used orally as a solid dosage forms. But this effect can be
reduce by solution system.
20. Disadvantage
Less stable in aqueous system. Incompatibility is faster in
solution than solid dosage form.
Patients have no accurate measuring device.
Accident breakage of container results in complete loss.
Solution often provide suitable media for the growth of micro
organisms.
The taste of a drug, which is often unpleasant, is always more
pronounced when in solution than in a solid form.
Bulky than tablets or capsule, so difficult to carry transport.
21. Monophasic liquid dosage forms
• It contain only one phase.
• It is represented by true solution.
• A true solution is a clear homogenous mixture that is prepared
by dissolving solute in a suitable solvent.
• Monophasic liquid dosage forms are – a)Syrup b)Elixirs
c)Solutions d) Linctuses
22. Syrup
It is a concentrated or saturated solutions of sucrose in purified
water.
The concentration of sucrose is 66.7% w/w & due to that it is a
viscous preparations.
The syrup which contains medical substance called as a
medicated syrup & those containing aromatic or flavored
substance known as a flavored syrup.
23. Elixirs
It is clear, sweetened, aromatic,
hydroalcholic preparations meant for
oral use.
The medicated elixirs are generally
contained potent drug like as
antibiotics, antihistamine or sedative ,
where as non–medicated elixirs
contained flavored.
The composition of elixirs contained
mainly as ethyl alcohol (active
ingredients),water, glycerin or
propylene glycol, coloring agent,
flavoring agent & preservative.
24. Linctuses
These are viscous liquid preparations
that’s are used for the treatment of
cough.
They contain one or more
medicaments which have demulcent,
sedative, expectorant action on the
mucus membrane of throat.
They are taken in small doses without
diluting with water to have prolonged
effect of medicines.
Simple syrup is used as a vehicle for
most of the linctuses.
25. The liquid which consist of two phases are known as a
biphasic liquid dosage forms.
They are sub categorized into two different forms namely as –
I) Emulsion
II) Suspension
In emulsion both phases are available in liquid where as in
suspension, finely divided solid particles are suspended in
liquid medium.
Biphasic liquid dosage forms
26. Emulsion
Emulsion is a biphasic liquid preparations containing two
immiscible liquid (Continuous Phase & dispersed phase) made
miscible.
The liquid which is converted into minute globules is called as
dispersed phase & the liquid in which the globules are
dispersed is called the continuous phase.
dispersed phase
continuous phase
Two Immiscible Liquids
Dispersed Phase
(Internal phase)
Continuous Phase
(External phase)
27. Types of emulsions
Simple type
Water in oil (w/o)
Oil in water (o/w)
Depending on globule size
Micro emulsion
Fine emulsion
Special type
Multiple emulsion (w/o/w, o/w/o)
28. Suspension
Suspensions are the biphasic liquid dosage forms of medicament in which
finely divided solid particles ranging from 0.5 to 5 micron are dispersed in a
liquid or semisolid vehicle, with aid of single or combination of suspending
agent.
In which solid particles acts as disperse phase where as liquid vehicle acts as
continuous phase
The external phase (suspending medium) is generally aqueous in some
instance, may be an organic or oily liquid for non oral use.
The particle size for non oral suspension is so important to avoid grittiness to
skin.
29. External liquid preparations
A) Applied on the skin
LOTIONS
Are usually aqueous, alcoholic or oily
liquid preparations.
They are intended for external
application without friction or
rubbing to the affected area
Usually applied with the help of some
absorbent material such as cotton
wool or gauze.
It is generally used to provide
cooling, soothing and protective &
antiseptic action.
30. LINIMENTS
Liniments are liquid or semi- liquid preparations
meant for external application to the skin.
They are usually applied to the skin with friction
& rubbing of the skin.
Are usually alcoholic and oily liquid preparations
(monophasic) or emulsion (biphasic).
Alcoholic liniments are used generally for their
rubefacient and counterirritant effects. Such
liniments penetrate the skin more readily than do
those with an oil base.
The oily liniments are milder in their action and
may function solely as protective coatings
Liniments should not be applied to skin that are
bruised or broken.
31. B) Instilled into body cavities
Ear drops
Nasal drops
Nasal Sprays
Inhalations
Douches
Enemas
32. Ear drops
These are the solutions of drugs that are instilled into ear
cavity with the help of dropper.
These are generally used for cleaning the ear, softening the
wax & for treating the mild infections.
The solutions is generally prepared in water, glycerin,
propylene glycol & dilute alcohol.
33. Nasal drops
Nasal drops are aqueous or liquid
paraffin solutions meant for instillation
into nostrils.
Drugs in solution may be instilled into
the nose from a dropper or from a
plastic squeeze bottle.
The drug may have a local effect, e.g.
antihistamine, decongestant.
Alternatively the drug may be absorbed
through the nasal mucosa to exert a
systemic effect.
34. douche
• A douche is a device used to introduce
a stream of water into the body for
medical or hygienic reasons, or the
stream of water itself.
• Douche usually refers to vaginal
irrigation, the rinsing of the vagina, but
it can also refer to the rinsing of any
body cavity.
• A douche bag is a piece of equipment
for douching—a bag for holding the
fluid used in douching.
35. C) Used in mouth
Gargles
Gargles are aqueous solutions used
for treating throat infection by
forcing air from lungs through the
gargle that is held in the throat.
dispensed in concentrated forms
with directions of dilution with
water before use
They are used into intimate contact
with the mucous membrane of throat
for few seconds, before they are
thrown out of the mouth.
They are also used for their
antiseptics, antibiotics anesthetics,
astringent,alkalinizing antifungal
action.
36. Mouth wash
These are aqueous solutions with
pleasant or acceptable taste & odour
These are used to make clean &
deodorise the buccal cavity or used
for oral hygiene and to treat
infections of the mouth.
They mainly contain antibacterial
agent, alcohol, glycerin, sweetening
agent, flavoring agent & colouring
agent.
37. Semisolid dosage forms
Semisolid dosage forms meant for external application
They contain one or more active ingredients dissolved or
uniformly dispersed in a suitable base and any suitable
excipients such as emulsifiers, viscosity-increasing agents,
antimicrobial agents, antioxidants, or stabilizing agents
Semisolid dosage forms subcategorized are as-
I) ointment
II) creams
III) paste
IV) Jellies
V) Suppositories
38. Ointment
Ointments are homogeneous semisolid
preparation meant for application to skin or
mucous membrane.
The ointments are mainly used for their
protective or emollient properties
39. Creams
Creams are homogeneous, semi-solid preparations consisting
of opaque emulsion systems
Cream is divided in to two types namely as
I) Aqueous creams
II) Oily creams
In case of aqueous creams the emulsions are o/w type & it is
relatively non greasy.
In case of oily creams w/o type & it is relatively greasy
The cream should be store in collapsible tube & supplied in
well closed container to prevent evaporation & contamination.
40. Pastes
Pastes are homogeneous, semi-solid
preparations containing high concentrations
of insoluble powdered substances (usually
not less than 20%) dispersed in a suitable
base.
They are mainly used as a antiseptic,
protective, soothing dressings.
Pastes should be stored & supplied in
containers made of materials which do not
allow absorption or diffusion of content.
41. Gel
Gels are usually transparent or
translucent,non-greasy semi-solid
preparations.
Gels are applied to the skin or certain
mucous membranes for protective,
therapeutic, or prophylactic purposes.
These are also used for lubricating
catheters, surgical gloves & rectal
thermometer.
42. New drug delivery system
With the advancement of pharmaceutical sciences, a new
concept have evolved various modern dosage forms &
methods of their administration. Some of the modern
dosage forms are
Implants
Films & strips
Liposome drug carriers
Controlled drug delivery modules
Erythrocytes
Nanoparticles
prodrugs
43. Implants
These are hypodermic tablets are placed under the skin by a
minor surgery in order to release drugs over prolonged periods
of time.
Now the magnetically controlled implants have been
developed.
These implants are useful in hormone therapy.
44. Films & strips
These are meant for topical application for slow release of drug over
predetermined period of time. Films & strips are more popular these days.
They are sub categorized in to following types namely as
Zero order release films
Buccal strips
Spray bandages
45. Liposome drug carriers
• Liposomes are defined as the nanosized vesicular structures
consisting of an aqueous core surrounded with phospholipid
layers
• These can transport both hydrophilic & hydrophobic drugs.
46. Controlled drug delivery modules
These are the device which are formed by embedding the
drug within a polymeric matrix so that it gets released slowly
to the body over a long period of time.
It will formed drug – polymer complex & may be formulated
in to tablet, capsule or any other suitable formulation.
The drugs is released from these modules by diffusion,
osmosis or chemical reactions.
These are applied to skin, implanted subcutaneously or
inserted into various body cavities.
47. Erythrocytes
Erythrocytes are tried in order to achieve controlled release of drugs.
It can allow a drug to circulate in the body for long period of time which help
slow release of the drugs in to serum.
Released erythrocytes are prepared by putting them in to a hypotonic medium.
So that they can easily swollen.
The aqueous solutions of the drug is added to the medium so that drugs gets in
to erythrocytes through open pores.
When isotonicity is adjusted the erythrocytes shrink, thus encapsulating the
drug with in them. These erythrocytes may be suspended in normal saline
solutions for preparing injections.